EP4480483A3 - Formes à l'état solide de sels de bélunosudil et de bélunosudil - Google Patents

Formes à l'état solide de sels de bélunosudil et de bélunosudil Download PDF

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Publication number
EP4480483A3
EP4480483A3 EP24204028.5A EP24204028A EP4480483A3 EP 4480483 A3 EP4480483 A3 EP 4480483A3 EP 24204028 A EP24204028 A EP 24204028A EP 4480483 A3 EP4480483 A3 EP 4480483A3
Authority
EP
European Patent Office
Prior art keywords
belumosudil
salts
solid state
state forms
processes
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP24204028.5A
Other languages
German (de)
English (en)
Other versions
EP4480483A2 (fr
Inventor
Polina Lapido
Inbal SHUMACHER
Ofir SHAUL
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Assia Chemical Industries Ltd
Original Assignee
Assia Chemical Industries Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Assia Chemical Industries Ltd filed Critical Assia Chemical Industries Ltd
Publication of EP4480483A2 publication Critical patent/EP4480483A2/fr
Publication of EP4480483A3 publication Critical patent/EP4480483A3/fr
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
EP24204028.5A 2020-07-22 2021-07-22 Formes à l'état solide de sels de bélunosudil et de bélunosudil Pending EP4480483A3 (fr)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US202063054918P 2020-07-22 2020-07-22
US202063075368P 2020-09-08 2020-09-08
US202063104329P 2020-10-22 2020-10-22
US202163137212P 2021-01-14 2021-01-14
EP21755332.0A EP4185580B8 (fr) 2020-07-22 2021-07-22 Formes solides de belumosudil et de sels de belumosudil
PCT/US2021/070924 WO2022020850A1 (fr) 2020-07-22 2021-07-22 Formes solides de belumosudil et de sels de belumosudil

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
EP21755332.0A Division-Into EP4185580B8 (fr) 2020-07-22 2021-07-22 Formes solides de belumosudil et de sels de belumosudil
EP21755332.0A Division EP4185580B8 (fr) 2020-07-22 2021-07-22 Formes solides de belumosudil et de sels de belumosudil

Publications (2)

Publication Number Publication Date
EP4480483A2 EP4480483A2 (fr) 2024-12-25
EP4480483A3 true EP4480483A3 (fr) 2025-02-26

Family

ID=77338971

Family Applications (2)

Application Number Title Priority Date Filing Date
EP21755332.0A Active EP4185580B8 (fr) 2020-07-22 2021-07-22 Formes solides de belumosudil et de sels de belumosudil
EP24204028.5A Pending EP4480483A3 (fr) 2020-07-22 2021-07-22 Formes à l'état solide de sels de bélunosudil et de bélunosudil

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP21755332.0A Active EP4185580B8 (fr) 2020-07-22 2021-07-22 Formes solides de belumosudil et de sels de belumosudil

Country Status (14)

Country Link
US (5) US11773083B2 (fr)
EP (2) EP4185580B8 (fr)
JP (3) JP2023535447A (fr)
KR (1) KR20230043910A (fr)
CN (2) CN119219610B (fr)
CA (1) CA3186800A1 (fr)
ES (1) ES3007246T3 (fr)
HR (1) HRP20241789T1 (fr)
HU (1) HUE069889T2 (fr)
IL (1) IL300040A (fr)
PL (1) PL4185580T3 (fr)
PT (1) PT4185580T (fr)
SI (1) SI4185580T1 (fr)
WO (1) WO2022020850A1 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230043910A (ko) 2020-07-22 2023-03-31 테바 파마슈티컬스 인터내셔널 게엠베하 벨루모수딜 및 벨루모수딜 염의 고체 상태 형태
WO2022170864A1 (fr) * 2021-02-09 2022-08-18 苏州科睿思制药有限公司 Forme cristalline du mésylate de beumosul, son procédé de préparation et son utilisation
CN115124514A (zh) * 2021-03-26 2022-09-30 广东东阳光药业有限公司 Kd-025的共晶及其制备方法
US20240343712A1 (en) * 2021-07-16 2024-10-17 Sandoz Ag Solid-state forms of 2-(3-(4-(1h-indazol-5-ylamino)quinazolin-2-yl)phenoxy)-n-isopropylacetamide methane sulfonic acid salt
WO2024000060A1 (fr) * 2022-06-30 2024-01-04 Apotex Inc Sels de bélumosudil, formes cristallines et compositions pharmaceutiques de ceux-ci et leur utilisation dans le traitement d'une maladie chronique du greffon contre l'hôte
WO2024063770A1 (fr) * 2022-09-21 2024-03-28 Kadmon Corporation, Llc Formulation liquide à base de belumosudil
WO2024100601A1 (fr) 2022-11-11 2024-05-16 Assia Chemical Industries Ltd. Formes à l'état solide de belumosudil et leurs procédés de préparation
CN117603194A (zh) * 2023-10-30 2024-02-27 南京科默生物医药有限公司 一种甲磺酸贝舒地尔的晶型及其制备工艺
WO2025257846A1 (fr) * 2024-06-14 2025-12-18 Natco Pharma Limited Procédé amélioré pour la préparation de mésylate de bélumosudil et de ses intermédiaires

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006105081A2 (fr) * 2005-03-25 2006-10-05 Surface Logix, Inc. Composes pharmacocinetiquement ameliores
EP3875078A1 (fr) * 2020-03-06 2021-09-08 Dompe' Farmaceutici S.P.A. Des composes pour pour le traitement de covid-19

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008054599A2 (fr) 2006-09-27 2008-05-08 Surface Logix, Inc. Inhibiteurs de la rho kinase
WO2012040499A2 (fr) 2010-09-22 2012-03-29 Surface Logix, Inc. Inhibiteurs métaboliques
CN113620933A (zh) 2012-10-05 2021-11-09 卡德门企业有限公司 Rho激酶抑制剂
US11311541B2 (en) 2014-04-09 2022-04-26 Kadmon Corporation, Llc Treatment of GVHD
CN106916145B (zh) 2017-03-06 2019-06-04 上海应用技术大学 SLx-2119的合成方法
CN114746412A (zh) * 2019-12-27 2022-07-12 广东东阳光药业有限公司 Kd-025的新晶型及其制备方法
KR20230043910A (ko) 2020-07-22 2023-03-31 테바 파마슈티컬스 인터내셔널 게엠베하 벨루모수딜 및 벨루모수딜 염의 고체 상태 형태
WO2022170864A1 (fr) 2021-02-09 2022-08-18 苏州科睿思制药有限公司 Forme cristalline du mésylate de beumosul, son procédé de préparation et son utilisation
CN114907325A (zh) * 2021-02-09 2022-08-16 苏州科睿思制药有限公司 Belumosudil甲磺酸盐的晶型及其制备方法和用途
CN115073430A (zh) * 2021-03-10 2022-09-20 苏州科睿思制药有限公司 Belumosudil甲磺酸盐的晶型及其制备方法和用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006105081A2 (fr) * 2005-03-25 2006-10-05 Surface Logix, Inc. Composes pharmacocinetiquement ameliores
EP3875078A1 (fr) * 2020-03-06 2021-09-08 Dompe' Farmaceutici S.P.A. Des composes pour pour le traitement de covid-19

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MINO R CAIRA ED - MONTCHAMP JEAN-LUC: "Crystalline Polymorphism of Organic Compounds", TOPICS IN CURRENT CHEMISTRY; [TOPICS IN CURRENT CHEMISTRY], SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP008166276, ISSN: 0340-1022, [retrieved on 19990226], DOI: 10.1007/3-540-69178-2_5 *

Also Published As

Publication number Publication date
CA3186800A1 (fr) 2022-01-27
US12157729B2 (en) 2024-12-03
ES3007246T3 (en) 2025-03-19
US20240124425A1 (en) 2024-04-18
KR20230043910A (ko) 2023-03-31
JP2023535447A (ja) 2023-08-17
US20250066333A1 (en) 2025-02-27
US20250066334A1 (en) 2025-02-27
CN116390918B (zh) 2024-12-24
JP2025113269A (ja) 2025-08-01
JP2026047356A (ja) 2026-03-13
PL4185580T3 (pl) 2025-04-14
WO2022020850A1 (fr) 2022-01-27
EP4185580B1 (fr) 2024-11-13
CN119219610A (zh) 2024-12-31
HRP20241789T1 (hr) 2025-03-14
EP4185580B8 (fr) 2024-12-18
SI4185580T1 (sl) 2025-05-30
IL300040A (en) 2023-03-01
EP4480483A2 (fr) 2024-12-25
CN116390918A (zh) 2023-07-04
CN119219610B (zh) 2026-03-06
PT4185580T (pt) 2025-01-16
US11773083B2 (en) 2023-10-03
US20230391755A1 (en) 2023-12-07
US11932627B2 (en) 2024-03-19
US20230117059A1 (en) 2023-04-20
EP4185580A1 (fr) 2023-05-31
HUE069889T2 (hu) 2025-04-28

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